Story of Brassaiopsis glomerulata
Brassaiopsisglomerulatais a member of the Araliaceae that occurs in south and southeast Asia. B. glomerulata is a large shrub or small tree with thorns on the stems, palmate leaves with 5–7 leaflets. [1]
This species has several reported traditional medicinal uses. [2] In Vietnam, the plant is used to treat rheumatism and back pain. In India, a group of indigenous tribes called the Nagas drank a juice extract of Brassaiopsis glomerulata bark to aid in digestion and to alleviate constipation. The Nagas also used a paste of the bark of Brassaiopsis glomerulata to treat bone fractures and sprains. This species is also used medicinally in China as one of several kinds of “tongcao”, which means unblocking herbs used to promote urination and assist in lactation. Owing to its use as a “tongcao”, Brassaiopsis glomerulata was then tested usingin vivo anti-inflammatory, antipyretic, and diuretic models.
The past history of medicinal use by human populations of Brassaiopsis glomerulata may be indicative of being safe when consumed. With the development of modern science, the strong aromatase inhibition of Brassaiopsis glomerulata extract was discovered by both enzyme- and cell-based assays, coupled with the possibility of a favorable safety profile, which both point to the potential for use of Brassaiopsis glomerulata for the hormone modulation.
Extractof Brassaiopsis glomerulata
Interested by the traditional use and novel discovery of Brassaiopsis glomerulata, several researchers investigate the components of it. Its compositions are mainly: [3]
• Acankoreoside A
• 3α-hydroxy-lup-20(29)-en-23,28-dioic acid
• 3α,11α-dihydroxy-23-oxo-lup-20(29)-en-28-oic acid
• Stigmasterol, 6β-hydroxystimasta-4-en-3-one, 7β-hydroxy-4,22-stigmastadien-3-one
• N-benzoyl-L-phenylalaninyl-N-benzoyl-L-phenylalaninate, N-acetyl-L-phenylalaninyl-N-benzoyl-L-phenylalaninate, and N-benzoyl-L-phenylalanine methyl ester
• Spinasterone and spinasterol
• Oleanolic acid
• (−)-dihydroactinidiolide
• (−)-dehydrololiolide
• 4-hydroxybenzaldehyde
• Linoleic acid (fatty acid)
Because little was known about the components of Brassaiopsis glomerulata, American researchers subjected it to examination [2]. They discovered that extracts of Brassaiopsis glomerulata leaves have an anti-oestrogenic effect. They isolated the ingredients in the extract and determined the anti-oestrogenic effect of each one. The researchers looked at whether the compounds could inhibit the aromatase that converting androstenedione into female hormones in test tubes trials, and whether they inhibited the conversion in live human cells. The researchers tested the plant ingredients at a concentration of 20ug/ml and meanwhile researchers compared their anti-oestrogenic effect with standard aromatase inhibitors: cytadren (AG) and letrozole (LET).
As the right figure show, the researchers isolated 13 compounds. Among them:
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showed the most significant aromatase inhibition properties. (−)-dehydrololiolide was found to be as effective as Letrozole, which is approved by FDA as non-steroidal aromatase inhibitor.
Aromatase Inhibition: a Favorable Property for Anabolism
As mentioned above, the attractive effect of Brassaiopsis glomerulata extract is due to its aromatase inhibition property. Aromatase is the enzyme responsible for catalyzing the last steps of biosynthesis of estrogens (estrone and estradiol) from androgens (androstenedione and testosterone). Inhibition of aromatase has been shown to reduce estrogen production throughout the body to nearly undetectable levels. [4]
Bodybuilders that take anabolic ingredients often use aromatase inhibitors in order to minimize or avoid estrogenic effects. Aromatase inhibitors can prevent elevated levels of testosterone from being converted to excess estrogen and have also been shown to reverse age-related decline in testosterone.
Reference
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2. Marcy J. Balunasa,b,d, Bin Sub, et. al. Isolation and Characterization of Aromatase Inhibitors from Brassaiopsis glomerulata (Araliaceae). Phytochem Lett. 2009 February 19; 2(1): 29–33.
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